Abstract: The present invention relates to a pharmaceutical formulation in powder form comprising amoxicillin, cineole and a pharmaceutically acceptable oil. The present formulation may also comprise clavulanic acid. It is intended for oral administration, preferably after suspension in an aqueous solvent. The present invention also relates to a combination of cineole and amoxicillin for use in the treatment of an infectious pathology, preferably a bacterial infection, in an individual. The present combination may also comprise a ?-lactamase inhibitor, preferably clavulanic acid. The combination according to the invention makes it possible in particular to combat infections caused by bacteria that are resistant to antibiotics, preferably to antibiotics of the ?-lactamine family.

Abstract: The disclosure discusses chiral dopants for liquid-crystalline materials. Chiral dopants can be bioreachable compounds, i.e. compounds produced from microbes through fermentation. Chiral dopants can also include bioreachable materials that are further modified by chemical synthetic steps. Chiral dopants as discussed herein can include biomolecules such as glycyrrhetinic acid (1), S-naringenin (2), shikimic acid (3), alpha-phellandrene (4), betulin (5), malic acid (6), valencene (7), or nootkatone (8), and any stereoisomers or chemically modified derivatives thereof. The disclosure further shows optical properties of such compounds in a liquid-crystalline material.

Abstract: The present invention provides an eye drop formulation in the form of a solution, comprising (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran or a pharmaceutically acceptable salt thereof; propylene glycol as a stabilizing agent; and a pH controlling agent in an aqueous medium, wherein the eye drop formulation has a pH ranging from 4.0 to 5.0. The eye drop formulation of the present invention can contain (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran or a pharmaceutically acceptable salt thereof in a high concentration; and has an excellent stability. In addition, the pharmaceutical product for preventing or treating macular degeneration according to the present invention can be stored for extended periods.

Abstract: The present invention provides a technique that allows a pharmaceutical composition, preferably for external use, containing luliconazole or the like to contain luliconazole or the like at a high concentration, and suppresses the precipitation thereof over time. The present invention uses a polyethylene glycol having an average molecular weight of 380 to 420 represented by a formula HOCH2(CH2OCH2)nCH2OH (where n is an integer), ethanol, benzyl alcohol, lactic acid, propylene carbonate, and acetone in combination with the luliconazole or the like.

Abstract: Provided is a method to identify subjects with inflammatory diseases, such as inflammatory bowel disease, for their suitability for treatment with antifungal compounds. The method comprises identification of loss-of-function in the gene CX3CR1.

Abstract: The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising at least one organic acid; at least one drug layer comprising trihexyphenidyl or a pharmaceutically acceptable salt thereof over the core; and a functional coat over the drug-layered core. The compositions of the disclosure provide extended release with reduced Cmax, a Cmin:Cmax ratio of ?0.4, Fluctuation Index of ?1, while providing and maintaining at least a minimum therapeutically effective plasma concentration, of the trihexyphenidyl or the pharmaceutically acceptable salt thereof for at least about 10 hours. The compositions of the disclosure improve solubility of the trihexyphenidyl or the pharmaceutically acceptable salt thereof at a pH of greater than or equal to 5, to provide and maintain at least a minimum effective concentration of the drug at such pH.

Abstract: Methods of treating glioblastoma are provided comprising: administering a therapeutically effective amount of azeliragon, or a pharmaceutically acceptable salt thereof, and co-administering an effective amount of radiation therapy (RT), to a patient who has been diagnosed with glioblastoma. In another aspect, methods are provided for treating grade I, grade II, and grade III gliomas, the method comprising administering a therapeutically effective amount of azeliragon, or a pharmaceutically acceptable salt thereof, and co-administering an effective amount of radiation therapy (RT), to a patient who has been diagnosed with glioma.

Abstract: The present invention relates to methods of treating coronavirus infections using compounds having anti-tubulin or tubulin disruption activity.

Abstract: Provided are 2-aminoimidazole-phenyl derivative compounds of Formula (I): which compounds are useful in methods of controlling microbial growth, such as by enhancing the effects of an antibiotic administered in combination with the compound. Compositions including these compounds, devices including these compounds, and methods of using the same are also provided.

Abstract: The present invention relates to metabolites of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl-amine. These metabolites may act as RAGE antagonists. These metabolites may also be useful in assays to measure the presence or amount of one or more metabolites of the parent compound in a sample.

Abstract: Inhibitors of oxidized low-density lipoprotein receptor 1 (LOX-1), compositions comprising inhibitors of LOX-1, and methods of using thereof are described.

Abstract: The invention relates to a method for treating or preventing nausea and vomiting. The method comprises administering an eye drop composition comprising palonosetron or a pharmaceutically acceptable salt thereof to the eye of the subject. The ocular administration results in fast systemic absorption, improved bioavailability compared to oral route and extended elimination time.

Abstract: A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and/or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and/or preparation of a drug with sedative, hypnotic and/or anesthetic effects and controlling the state of epilepsy.

Abstract: There are provided compounds, their preparation and their use in the treatment of KRAS-driven cancers. The compounds according to the invention (general formula Class III) disrupt dimerization of KRAS and are inhibitors of KRAS mutants such as KRAS G12D, KRAS G12V and KRAS 12C. Embodiments of the compounds according to the invention are selective inhibitors of KRAS mutants over the wild-type (WT) KRAS.

Abstract: The present disclosure relates to a new salt of escitalopram and its solid state forms, processes for the preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention provides for methods for treating pancreatic cancer, reducing or inhibiting pancreatic tumor cells, inhibiting or treating pancreatic cancer metastases, and inhibiting pancreatic cancer stem cell growth in a subject by administering a cholinergic agonist.

Abstract: Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

Abstract: The invention provides compositions and methods for treating neurological disorders, such as amyotrophic lateral sclerosis, frontotemporal degeneration, and Alzheimer's disease, among others. Using the compositions and methods described herein, a patient having a neurological disorder, such as a neurological disorder associated with TAR-DNA binding protein (TDP)-43 aggregation, may be administered an inhibitor of cytochrome P450 (CYP450) isoform 51A1 (CYP51A1), also referred to herein as lanosterol 14-alpha demethylase, so as to treat an underlying etiology of the disorder and/or to alleviate one or more symptoms of the disease. The inhibitor of CYP51A1 may be a small molecule, anti-CYP51A1 antibody or antigen-binding fragment thereof, or a compound, such as an interfering RNA molecule, that attenuates CYP51A1 expression.

Abstract: The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by absormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.

Abstract: An amide derivative inhibitor and a preparation method and an application thereof. Specifically relating to the compound shown in general formula (I), a preparation method for same, a pharmaceutical composition comprising said compound, and an application of same as an ASK inhibitor for the treatment of neurodegenerative disease, cardiovascular disease, inflammation, autoimmune and metabolic disease, each of the substituents in the general formula (I) being as defined in the description.

Abstract: The present invention provides a technique that allows a pharmaceutical composition, preferably for external use, containing luliconazole or the like to contain luliconazole or the like at a high concentration, and suppresses the precipitation thereof over time. The present invention uses a polyethylene glycol having an average molecular weight of 380 to 420 represented by a formula HOCH2(CH2OCH2)nCH2OH (where n is an integer), ethanol, benzyl alcohol, lactic acid, propylene carbonate, and acetone in combination with the luliconazole or the like.

Abstract: The present invention includes compositions and methods for providing a therapeutically acceptable dose of an active pharmaceutical agent for once a day delivery of the active pharmaceutical compound in an amount effective to treat at least one of: Sjogren's syndrome, Xerostomia, dry mouth, hypo-salivation, or dental carries due to reduced or compromised salivation, wherein both the peak and trough times in the blood level at 8 hours is greater than 25% of the peak value in the blood level concentration.

Abstract: The present invention describes the use of a 5HT3-antagonist, in combination with pyridostigmine, to facilitate the symptomatic treatment of mammalian subjects, and particularly humans, dogs, and cats, suffering from a myasthenic syndrome, notably myasthenia gravis, by providing a therapeutically effective pyridostigmine bromide daily dose without the typical adverse effects.

Abstract: A compound of Formula (I) or (II), for treating or preventing an HCV infection in a subject.

Abstract: The invention relates to the field of medicine and concerns an agent that stimulates tissue regeneration and the recovery of diminished tissue and organ function. A medicinal agent for the treatment and/or prophylaxis of a pathological condition selected from the group including metabolic syndrome, impaired glucose tolerance, hepatitis, particularly chronic hepatitis and toxic hepatitis, idiopathic pulmonary fibrosis (IPF), emphysema of the lungs, chronic obstructive pulmonary disease (COPD) and cachexia, particularly as a result of impaired glucose tolerance, pulmonary fibrosis, chronic obstructive pulmonary disease, cancer and other diseases, is proposed in the form of an agent based on Treamide. The latter is a bisamide derivative of dicarboxylic acid of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The disclosure relates to a composition for improving aortic endothelial cell function and use thereof. The composition includes acetic acid, lactic acid, polyoxyethylene castor oil, and disodium alkyl polyoxyethylene sulfosuccinate. The composition is capable of inhibiting inflammatory response of the human aortic endothelial cells caused by saturated fatty acids, increasing a mitochondrial respiration and metabolism of vascular endothelial cells, and preventing an occurrence and progression of atherosclerosis. The composition is capable of reducing human aortic endothelial inflammation caused by saturated fatty acids, for example, reducing the mRNA levels of interleukin-6 (IL-6) and matrix metalloproteinase-1 (MMP-1), and is capable of effectively protecting the function of mitochondria in human aortic endothelium from being damaged by saturated fatty acids, for example, increasing the expression of mitochondrial complexes I and III and mitochondrial metabolism-associated Foxo1.

Abstract: The present invention provides a process for purifying (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran, comprising converting an amorphous (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran to a crystalline form thereof. And also, the present invention provides a novel crystalline form of (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazol-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyran and processes for preparing the same.

Abstract: The present invention relates to novel therapeutic agents suitable for use in the treatment of mammalian disease and in particular to novel therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes.

Abstract: Described herein are compound for the modulation of the G-CSF receptor. The compounds may act as agonists, antagonists, and/or mixed or partial agonists/antagonists of G-CSF. Further provided herein are methods of treating a condition, including, for example, a neurodegenerative disease, by administering a compound as detailed herein.

Abstract: The present invention relates to compositions and methods for the treatment of prostate cancer. The present invention relates to polyamides and prostate agents, for example, to inhibit an androgen receptor signaling axis, and the use of these compositions in the treatment of prostate cancer.

Abstract: The present invention relates to compounds having a selective FKBP51 ligand scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said selective FKBP51 ligand compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Abstract: The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, L, Y, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: The invention relates to the field of medicine and concerns an agent that stimulates tissue regeneration and the recovery of diminished tissue and organ function. A medicinal agent for the treatment and/or prophylaxis of a pathological condition selected from the group including metabolic syndrome, impaired glucose tolerance, hepatitis, particularly chronic hepatitis and toxic hepatitis, idiopathic pulmonary fibrosis (IPF), emphysema of the lungs, chronic obstructive pulmonary disease (COPD) and cachexia, particularly as a result of impaired glucose tolerance, pulmonary fibrosis, chronic obstructive pulmonary disease, cancer and other diseases, is proposed in the form of an agent based on Treamide. The latter is a bisamide derivative of dicarboxylic acid of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Benzimidazole derivatives of Formula I, that modulate the activity of ACSS2 are disclosed for therapeutic use. The fused imidazole ring of the compounds disclosed has a diarylmethyl or diarylmethanol moiety attached at the 2-position and the as compounds have at least one other substituent at the 5 or 6 position of the benzimidazole. Also disclosed are methods of using the benzimidazole compounds for the treatment of diseases or disorders, such as cancer.

Abstract: The present invention relates to compositions containing polymeric, ionic compounds comprising imidazolium groups. In particular, it relates to the use of polymeric, ionic compounds comprising imidazolium groups in personal care compositions and/or in biocide compositions.

Abstract: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.

Abstract: Ophthalmic composition for the correction of presbyopia. Composition consisting of 2% Pilocarpine, characterized by being diluted to 1% with sterile Balanced Salt Solution (BSS), obtaining 1% pilocarpine (2.5 ml)+bromfenac, 1.8 mgrs of bromfenac (2.5 ml)+sterile Balanced Salt Solution (BSS) (2.5 ml), finally obtaining eye drops of 7.5 ml. It is also possible to obtain a 1.5% and 2% pilocarpine.

Abstract: A medicinal preparation for preventing and/or treating psychoneurotic diseases such as integration dysfunction and Alzheimer's disease which contains tropisetron or its pharmaceutically acceptable salt as the active ingredient.

Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

Abstract: The disclosure relates to ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt. Aspects of the disclosure further relate to uses and preparations of ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt, for correcting presbyopia and other ocular conditions in a subject.

Abstract: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

Abstract: Aerosol formulations of ondansetron useful for pulmonary delivery are provided. The formulations are useful in the reduction, elimination or prevention of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Also provided are novel methods to treat chemotherapy-induced nausea and vomiting (CINV), radiation-induced nausea and vomiting (RINV), and post-operative nausea and vomiting (PONV) using the inhalation formulations.

Abstract: The present invention relates to methods of treatment using [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl amine (“COMPOUND I”) or a pharmaceutically acceptable salt thereof. In various embodiments, the methods of treatment include treatment of mild-to-moderate dementia of Alzheimer's type, diabetes, insomnia, and other indications. The present invention also relates to pharmaceutical compositions comprising COMPOUND I or a pharmaceutically acceptable salt thereof.

Abstract: Provided are methods of enhancing an immune response and methods for reducing the recruitment of monocytes to a lymph node by administering to an individual an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an antigen. The invention also provides relate methods for amplifying vaccine immunity by administering to an individual an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an vaccine. The invention also provides related methods of inhibiting tumor growth and metastasis by administering to an individual with cancer an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an anti-tumor preparation. In addition, related compositions comprising an ARB or a compound of Formula (I) and an antigen, vaccine, or anti-tumor preparation are provided.

Abstract: An object is to provide a crystal having a new crystal habit of luliconazole and expand the possibility of application to pharmaceuticals. Disclosed is a crystal of luliconazole having such a crystal habit that (020) plane is a specific crystal growth surface.

Abstract: The object of the present invention is to provide a fundamental therapy to mitochondrial genetic diseases caused by mutation of the mitochondrial (mt)DNA, and a pharmaceutical composition used for the same. The object can be solved by a polyamide compound binding to a target double-stranded mtDNA comprising A/T pair consisting of first A of the following sense-stranded DNA and the corresponding T, A/T pair consisting of 8th A of the following sense-stranded DNA and the corresponding T, G/C pair consisting of 9th G of the following sense-stranded DNA and the corresponding C, G/C pair consisting of 14th G of the following sense-stranded DNA and the corresponding C, T/A pair consisting of 15th T of the following sense-stranded DNA and the corresponding A, or the like, in the double-stranded DNA consisting of the sense-stranded DNA having base sequence of 5?-ATGGCAGAGCCCGGTAATCGCATAA-3? (SEQ ID NO: 1) and the antisense-stranded DNA having base sequence of 5?-TTATGCGATTACCGGGCTCTGCCAT-3? (SEQ ID NO: 2).

Abstract: The present invention belongs to the field of chemical pharmaceuticals, and specifically relates to compounds represented by formula I having a 9,9,10,10-tetrafluoro-9,10-dihydrophenanthrene structure and being able to inhibit hepatitis C virus activity, or a pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug of said compounds, a pharmaceutical composition containing said compounds, and an application of said compounds or composition in the preparation of a drug. The compounds of the present invention have a good HCV inhibitory effect.

Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.

Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.